化合物 T10946 T10946

Product Introduction
Bioactivity


英文名: D4-abiraterone

描述: D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.

体外活性: D4-Abiraterone (D4A) (10 mM) almost completely prevented the conversion of D4-androstenedione (AD) to 5α-androstanedione and other 5α-reducing androgens. D4-Abiraterone has greater affinity for androgen receptor (AR) than mutant (expressed in LNCaP, half maximum inhibitory concentration (IC50 = 5.3 nM)) and wild type (expressed in LAPC4, IC50 = 7.9 nM) Abiron (IC50 = 418 and> 500 nM, respectively). Compared with Abi, D4-abiraterone significantly inhibited the expression of PSA, TMPRSS2 and FKBP5 in LNCAP, LAPC4 and C4-2 cell lines. D4-Abiraterone also suppressed AR target gene expression in a dose-dependent manner.

体内活性: In preventing the conversion of 3β-hydroxysteroid dehydrogenase (3βHSD) from dehydroepiandrosterone (DHEA) to D4-androstenedione (AD) in LNCaP and VCaP xenografts, D4-Abiraterone (D4A) The effect is ten times higher than that of Abiron. In LNCaP and VCaP xenografts, AD accumulation was blocked at 48 h, and 0.1 μMD4-Abiraterone was equivalent to 1 μMAbi. Compared with the Abirate acetate group, the progress of the D4-Abiraterone group was significantly delayed (P = 0.011). Compared with abirate acetate, D4-Abiraterone treatment can increase progression-free survival .

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (143.89 mM)


关键字: D4-abiraterone | CB7627 | CB 7627 | D4abiraterone | D-4-abiraterone | D4 abiraterone | delta4-Abiraterone

相关产品: p,p'-DDE | Zanoterone | SK33 | RU 59063 | GSK-2881078 | Chlormadinone acetate | S-23 | MK-0773 FA | DSRM-3716 | BMS-641988

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